Results 221 to 230 of about 830,364 (264)
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G-protein-coupled receptors and cancer
Nature Reviews Cancer, 2007G-protein-coupled receptors (GPCRs), the largest family of cell-surface molecules involved in signal transmission, have recently emerged as crucial players in tumour growth and metastasis. Malignant cells often hijack the normal physiological functions of GPCRs to survive, proliferate autonomously, evade the immune system, increase their blood supply ...
Robert T, Dorsam, J Silvio, Gutkind
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G Protein-Coupled Receptor Pharmacogenetics
2008Common G protein-coupled receptor (GPCR) gene variants that encode receptor proteins with a distinct sequence may alter drug efficacy without always resulting in a disease phenotype. GPCR genetic loci harbor numerous variants, such as DNA insertions or deletions and single-nucleotide polymorphisms that alter GPCR expression and function, thereby ...
Miles D, Thompson +2 more
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Dimerization of G-Protein-Coupled Receptors
Journal of Medicinal Chemistry, 2001The evolutionary trace (ET) method, a data mining approach for determining significant levels of amino acid conservation, has been applied to over 700 aligned G-protein-coupled receptor (GPCR) sequences. The method predicted the occurrence of functionally important clusters of residues on the external faces of helices 5 and 6 for each family or ...
M K, Dean +8 more
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Deorphanization of G-Protein-Coupled Receptors
2007G-protein-coupled receptors constitute one of the major families of drug targets. Orphan receptors, for which the ligands and function are still unknown, are an attractive set of future targets for presently unmet medical needs. Screening strategies have been developed over the years in order to identify the natural ligands of these receptors.
Parmentier, Marc, Detheux, Michel
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G-Protein-Coupled Receptor Microarrays
ChemBioChem, 2002Membrane-bound proteins represent the single most important class of drug targets. Arraying these proteins is difficult because they typically need to be embedded in membranes to maintain their correctly folded conformations. We describe here the fabrication of microarrays consisting of G-protein-coupled receptors (GPCRs)--the single largest family of ...
Ye, Fang +2 more
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G-protein coupled receptors in bone
Frontiers in Bioscience, 1998The skeleton is a dynamic structure that undergoes continuous remodeling, a prerequisite to meeting the constant loading demands placed upon it. This process is controlled by a multitude of systemic and local factors which interact with receptors presented on the surface of both osteoblasts and osteoclasts; the osteogenic and osteolytic cells of bone ...
W B, Bowler, J A, Gallagher, G, Bilbe
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Fingerprinting G-protein-coupled receptors
"Protein Engineering, Design and Selection", 1994Recently we reported the design of a discriminating fingerprint for rhodopsin-like G-protein-coupled receptors (GPCRs). The fingerprint encodes the seven putative membrane-spanning motifs and was potently diagnostic of all GPCRs (52 in all) in version 8.1 of the OWL composite sequence database, readily distinguishing them from all other integral ...
T K, Attwood, J B, Findlay
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Activation of G Protein–Coupled Receptors
2007G protein-coupled receptors (GPCRs) mediate responses to hormones and neurotransmitters, as well as the senses of sight, smell, and taste. These remarkably versatile signaling molecules respond to structurally diverse ligands. Many GPCRs couple to multiple G protein subtypes, and several have been shown to activate G protein-independent signaling ...
Xavier, Deupi, Brian, Kobilka
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Efficacy at g-protein-coupled receptors
Nature Reviews Drug Discovery, 2002At present, the drug-discovery process centres on ligands that either block or produce physiological responses. However, there are therapeutic uses for ligands that do neither of these things, but which still affect receptors in other ways. This review discusses the intimate relationship between the affinity of a ligand for its receptor, and the ...
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Downregulation of G protein-coupled receptors
Current Opinion in Neurobiology, 2000Major advances have been made in understanding mechanisms mediating downregulation of G protein-coupled receptors. Recent studies emphasize the role of multiple proteolytic mechanisms in downregulation. A specific mechanism of downregulation, mediated by endocytosis of receptors via clathrin-coated pits followed by sorting to lysosomes, has been ...
P, Tsao, M, von Zastrow
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